Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TTNXLKE)

• DTT Name: 5-HT 3 receptor (5HT3R) DTT Info
• Gene Name: 5HT3R

Molecule-Related Drug & Molecule List

4 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Granisetron	DMIUW25	Malignant glioma	2A00.0	Approved	[1]
Ondansetron	DMOTQ1I	Chemotherapy-induced nausea	MD90	Approved	[2]
Ramosetron	DMH7GN8	Diarrhea-predominant irritable bowel syndrome	DD91.01	Approved	[3]
Y-25130	DMDPM7R	Nausea and vomiting	MD90	Approved	[4]

16 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lerisetron	DMOTCIU	Nausea	MD90	Phase 3	[5]
LITOXETINE	DMKZRBP	Mood disorder	6A60-6E23	Phase 3	[6]
Pancopride	DMIRYU9	Nausea	MD90	Phase 3	[7]
Renzapride	DM7HQNX	Irritable bowel syndrome	DD91.0	Phase 3	[8]
Zatosetron maleate	DMWDEFC	Anxiety disorder	6B00-6B0Z	Phase 3	[9]
AD04	DMLV9GS	Alcohol dependence	6C40.2	Phase 2	[10]
DDP-225	DM9REBL	Irritable bowel syndrome	DD91.0	Phase 2	[11]
KB-6806	DMZ4MCG	Chemotherapy-induced nausea	MD90	Phase 2	[5]
Lintopride	DMSHGWN	Nausea	MD90	Phase 2	[12]
Pumosetrag	DMBUSNL	Irritable bowel syndrome	DD91.0	Phase 2	[13]
ADR-851	DM6NUCA	Nausea and vomiting	MD90	Phase 1	[14]
BIMU-1	DMBTSZD	Cognitive impairment	6D71	Phase 1	[15]
CVN058	DMTSIYZ	Schizophrenia	6A20	Phase 1	[16]
ITASETRON	DMY1DFK	Nausea	MD90	Phase 1	[11]
TAK-058	DMX9EA0	Schizophrenia	6A20	Phase 1	[17]
Tedatioxetine	DMV5LGJ	Generalized anxiety disorder	6B00	Phase 1	[11]

17 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
RG-12915	DMXV28I	Nausea	MD90	Discontinued in Phase 3	[18]
BRL-46470	DMIHSOG	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 2	[19]
DAT-582	DMY3M0J	Nausea	MD90	Discontinued in Phase 2	[20]
E-3620	DMWF95G	Gastric motility disorder	DA21	Discontinued in Phase 2	[11]
Fabesetron	DMMSFK0	Irritable bowel syndrome	DD91.0	Discontinued in Phase 2	[21]
Lurosetron	DMYR2U3	Vomiting	MD90	Discontinued in Phase 2	[22]
SR-57227	DMV4FT2	Major depressive disorder	6A70.3	Discontinued in Phase 2	[23]
Mirisetron maleate	DMC2V5J	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 1	[24]
SEP-226332	DMCQI25	Obstructive sleep apnea	7A41	Discontinued in Phase 1	[25]
WAY-100289	DM3GD7V	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 1	[26]
BP4.879a	DMN8FAG	Schizophrenia	6A20	Terminated	[27]
CR-3124	DM1MBG9	Substance use disorder	6C4Z	Terminated	[28]
GK-128	DM4RKDU	Vomiting	MD90	Terminated	[29]
GR-65630	DMRPE3D	Vomiting	MD90	Terminated	[30]
SC-52150	DMKWJ59	Vomiting	MD90	Terminated	[31]
SDZ-ICM-567	DMN5IY7	Anxiety disorder	6B00-6B0Z	Terminated	[32]
SRSS-021	DM8MZWR	Vomiting	MD90	Terminated	[33]

6 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(R)-zacopride	DMT6J51	Discovery agent	N.A.	Investigative	[34]
BRL 43694A	DMTM7W0	Discovery agent	N.A.	Investigative	[35]
Ciproxifan	DM9N8WM	Dementia	6D80-6D86	Investigative	[36]
S-21007	DMOJ9N6	Discovery agent	N.A.	Investigative	[37]
SC-52491	DMJ576C	Discovery agent	N.A.	Investigative	[38]
SC-54750	DMEUTXG	Discovery agent	N.A.	Investigative	[38]

References

• [1] New approaches to chemotherapy-induced nausea and vomiting: from neuropharmacology to clinical investigations. Cancer J. 2006 Sep-Oct;12(5):341-7.
• [2] Treatment of pruritus in chronic liver disease with the 5-hydroxytryptamine receptor type 3 antagonist ondansetron: a randomized, placebo-controlled, double-blind cross-over trial. Eur J Gastroenterol Hepatol. 1998 Oct;10(10):865-70.
• [3] Inhibitory effect of YM060 on 5-HT3 receptor-mediated depolarization in colonic myenteric neurons of the guinea pig. Eur J Pharmacol. 1995 Sep 5;283(1-3):107-12.
• [4] The antiemetic profile of Y-25130, a new selective 5-HT3 receptor antagonist. Eur J Pharmacol. 1991 Apr 24;196(3):299-305.
• [5] Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.
• [6] Litoxetine: a selective 5-HT uptake inhibitor with concomitant 5-HT3 receptor antagonist and antiemetic properties. Eur J Pharmacol. 1993 Mar 2;232(2-3):139-45.
• [7] Pancopride, a potent and long-acting 5-HT3 receptor antagonist, is orally effective against anticancer drug-evoked emesis. Eur J Pharmacol. 1992 Nov 10;222(2-3):257-64.
• [8] Pharmacology and metabolism of renzapride : a novel therapeutic agent for the potential treatment of irritable bowel syndrome. Drugs R D. 2008;9(1):37-63.
• [9] Pilot study of zatosetron (LY277359) maleate, a 5-hydroxytryptamine-3 antagonist, in the treatment of anxiety. J Clin Psychopharmacol. 1999 Apr;19(2):125-31.
• [10] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [11] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [12] The effects of lintopride, a 5HT-4 antagonist, on oesophageal motility. Aliment Pharmacol Ther. 1995 Oct;9(5):563-9.
• [13] Novel partial 5HT3 agonist pumosetrag reduces acid reflux events in uninvestigated GERD patients after a standard refluxogenic meal: a randomized, double-blind, placebo-controlled pharmacodynamic study.Neurogastroenterol Motil.2014 Jan;26(1):13-20.
• [14] Analgesic effects of S and R isomers of the novel 5-HT3 receptor antagonists ADR-851 and ADR-882 in rats. Eur J Pharmacol. 1991 Oct 29;204(1):117-9.
• [15] Gastroprokinetic properties of the benzimidazolone derivative BIMU 1, an agonist at 5-hydroxytryptamine4 and antagonist at 5-hydroxytryptamine3 receptors. Naunyn Schmiedebergs Arch Pharmacol. 1994 Apr;349(4):338-45.
• [16] Clinical pipeline report, company report or official report of Cerevance.
• [17] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040805)
• [18] Cataractogenesis in rats induced by in utero exposure to RG 12915, a 5-HT3 antagonist. Fundam Appl Toxicol. 1995 Sep;27(2):270-6.
• [19] Evidence that the atypical 5-HT3 receptor ligand, [3H]-BRL46470, labels additional 5-HT3 binding sites compared to [3H]-granisetron. Br J Pharmacol. 1995 Sep;116(2):1781-8.
• [20] 5-HT3 receptor antagonist effects of DAT-582, (R) enantiomer of AS-5370. Eur J Pharmacol. 1992 Jun 17;216(3):435-40.
• [21] Pharmacological characterization of FK1052, a dihydropyridoindole derivative, as a new serotonin 3 and 4 dual receptor antagonist. J Pharmacol Exp Ther. 1993 May;265(2):752-8.
• [22] US patent application no. 7,932,267, Use of α-glucosidase inhibitors to treat alphavirus infections.
• [23] Antidepressant-like effects of SR 57227A, a 5-HT3 receptor agonist, in rodents. J Neural Transm Gen Sect. 1995;102(2):83-90.
• [24] The effects of 5-HT3 receptor antagonists on cognitive performance in aged monkeys. Neurobiol Aging. 1997 Jan-Feb;18(1):21-8.
• [25] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020129)
• [26] The selective 5-HT3 receptor antagonist, WAY100289, enhances spatial memory in rats with ibotenate lesions of the forebrain cholinergic projection system. Psychopharmacology (Berl). 1995 Feb;117(3):318-32.
• [27] 5-HT(3A) receptor subunit is required for 5-HT3 antagonist-induced reductions in alcohol drinking. Neuropsychopharmacology. 2004 Oct;29(10):1807-13.
• [28] Physicochemical and biopharmaceutical characterization of endo-2-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1H-benz[e]isoindol-1-one (CR312... J Pharm Sci. 2006 Dec;95(12):2706-21.
• [29] Effect of a novel 5-hydroxytryptamine3 (5-HT3) receptor antagonist, GK-128, on 5-HT3 receptors mediating contractions and relaxations in guinea-pig distal colon. Gen Pharmacol. 1997 Sep;29(3):353-9.
• [30] Binding of the 5-HT3 ligand, [3H]GR65630, to rat area postrema, vagus nerve and the brains of several species. Eur J Pharmacol. 1989 Jan 10;159(2):157-64.
• [31] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001830)
• [32] Microdialysis sampling to determine the pharmacokinetics of unbound SDZ ICM 567 in blood and brain in awake, freely-moving rats. Pharm Res. 1995 Feb;12(2):291-4.
• [33] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019090)
• [34] R-zacopride, a 5-HT3 antagonist/5-HT4 agonist, reduces sleep apneas in rats. Pharmacol Biochem Behav. 2001 May-Jun;69(1-2):283-9.
• [35] BRL 43694A--a 5-hydroxytryptamine receptor blocker as an antiemetic in cytostatic therapy. Schweiz Med Wochenschr. 1989 Jun 10;119(23):831-4.
• [36] The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20.
• [37] Effects of S-21007, a potent 5-HT3 partial agonist, in mouse anxiety. Zhongguo Yao Li Xue Bao. 1999 Sep;20(9):805-12.
• [38] Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5509-12.